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Pharmacology > PP- Antiprotozoal drugs > Flashcards

PP- Antiprotozoal drugs Flashcards

1
Q

What are the main protozoan infections in humans?

A
  • malaria
  • amoebiasis
  • pneumocystis infection
  • trypanosomiasis
  • leishmanisasis
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2
Q

What is malaria?

A
  • it is a mosquito-borne disease caused by various Plasmodium species
  • a major killer in the developing world
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3
Q

Which Plasmodium species cause most of the mortality of the malaria patients?

A

Plasmodium falciparum

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4
Q

Who ar ein the risk group of Plasmodium falciparum ?

A

the greatest risk, for children under 5 years of age and to all non-immune individuals

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5
Q

How are the parasite that cause malaria transmitted to humans?

A

the parasites (Plasmodium) are transmitted to humans by the bite of infected female Anopheles mosquito vector

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6
Q

Which Plasmodium species cause malaria?

A
  • P. falciparum
  • P. vivax
  • P. ovale
  • P. malariae
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7
Q

How are antimalarials categorized?

A

according to the stage of the parasite that they affect

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8
Q

P. vivax

A

gives rise to hypnozoites in the liver; these lie dormant and can produce relapses months or years later

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9
Q

P. falciparum

A

does not form hypnozoites and thus has no exo-erythrocytic stage

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10
Q

P. malariae

A
  • is rare

- has a 72-h cycle (quartan malaria) and also has no exo-erythrocytic stage

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11
Q

What does chloroquine do?

A

reduces the necessary digestion of haemoglobin by the plasmodium by inhibiting the parasite´s haem polymerase

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12
Q

What is haem polymerase?

A

it is the enzyme that inactivates the toxic free heam generated by the plasmodium

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13
Q

How is chloroquine given?

A
  • usually orally (half-life 0.5h)

- injection

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14
Q

How is chloroquine distributed?

A

it is widely distributed in the body but much is concentrated in the parasite cells

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15
Q

What are the unwanted effects of chloroquine?

A
  • nausea
  • vomiting
  • dizziness
  • large doses can cause retinopathy and bolus injections can cause dysrythmias
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16
Q

Which species of Plasmodium are resistant to chloroquine?

A
  • P. falciparum is resistant in most parts of the world

- P. vivax is resistant i some places

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17
Q

Schizonticide def:

A

an agent selectively destructive of the schizont of a sporozoan parasite

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18
Q

What does the blood schizonticide act on?

A

they act on the asexual erythrocytic stage to interrupt schizogony and thus terminate clinical attacs

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19
Q

How are blood schizonticide divided?

A
  1. rapid-acting blood schizonticide

2. slow-acting blood schizonticide

20
Q

Give examples of rapid-acting blood schizonticide?

A
  • quinine
  • chloroquine
  • mefloquine
21
Q

Give examples of slow-acting blood schizonticide?

A
  • sulfonamide

- pyrimethamine

22
Q

How is halofantrine given?

A
  • orally (half-life 30 days)

- the parent drug have a half-life of 1-2 days and the active metabolite 3-5 days

23
Q

What are the unwanted effects of using halofantrine?

A
  • GI tract disturbances

- occasionally cardiac dysrhythmias

24
Q

How is mefloquine given?

A
  • orally (half-life 30 days)

- slow onset of action

25
Q

How does the mefloquine work?

A

like, chloroquine, it inhibits haem polymerase

26
Q

What are the unwanted effects of using mefloquine?

A
  • GI tract disturbances

- may produce neuropsyciatric symptoms

27
Q

How is quinine given?

A
  • orally (half-life 10h)

- can be given by IV infusion

28
Q

What is quinine used with?

A
  • doxycycline and either
    • dapsone (given orally, half life 24-48h)
    • sulfadoxine, a long-acting sulfonamide (half-life 8 days)
29
Q

What are the unwanted effects of using quinine?

A
  • GI upset
  • tinnitus
  • headache
  • blurred vision
  • allergic reaction
  • large doses affect the heart (dysrythmias) and/ or the CNS (delirium)
30
Q

What is pyrimethamine?

A

a folate antagonist

31
Q

What does the pyrimethamine do?

A

inhibits folate utilization having greater affinity for the plasmodial than for the mammalian system

32
Q

What is pyrimethamine used with?

A
  • sulfadoxine, slow-acting (half-life 4 days). It has few unwanted effects
33
Q

Proguanil:

A
  • similar action of pyrimethamine

- slow-acting schizonticide (half-life 16h) with some action on the pre-erythrocytic stage of P. vivax

34
Q

How is proguanil given?

A

given orally

35
Q

How is primaquine given?

A
  • orally

- half-life 3-6h

36
Q

What is primaquine usually given with?

A

chloroquine

37
Q

What are the unwanted effects of primaquine?

A

it can cause hemolysis in individuals with genetic deficiency of red cell glucose 6-phosphate dehydrogenase

38
Q

What is doxycycline?

A
  • broad-spectrum tetracycline antibiotic

- acts by inhibiting plasmodial protein synthesis

39
Q

What is artemether?

A

a semi-synthetic derivative of artemisin

40
Q

What is artemether?

A

a compound extracted from a shrub used in traditional Chinese medicine

41
Q

How is artemether given?

A
  • orally
  • rectally
  • IM
42
Q

artemether mechanism of action:

A
  • concentrated in parasitic cells where it generates reactive oxygen species; and may inhibit a calcium transporter
  • inhibits hemoglobin degradation in the parasite
43
Q

When is artemether used?

A

in combination therapy only!

44
Q

What are the unwanted effects of artemether?

A

neurotoxicity can occur with high doses

45
Q

What causes amoebiasis?

A

ingestion of the cysts of Entamoeba histolytica

46
Q

How does the cysts of Entamoeba histolytica develop in the body?

A

the cyst develop in the GI tract into motile trophozoites which can invade the intestinal wall

Pharmacology (11 decks)

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